Tarawneh Amer H, Al-Momani Lo Ay A, León Francisco, Jain Surenda K, Gadetskaya Anastassiya V, Abu-Orabi Sultan T, Tekwani Babu L, Cutler Stephen J
Department of BioMolecular Sciences, University of Mississippi, University, MS 38677, USA.
Department of Chemistry, Tafila Technical University, Tafila, P.O. Box 179, Jordan.
Med Chem Res. 2018 Apr;27(4):1269-1275. doi: 10.1007/s00044-018-2146-4. Epub 2018 Feb 27.
A series of isoxazole and triazole derivatives, with interesting bioactive scaffolds, were examined for their antibacterial, antifungal, and antiprotozoal activities. These compounds exhibited antitrypanosomal activity comparable to difluoromethylornithine (DMFO), a drug used in the treatment of human African trypanosomiasis. Isoxazole analogues , and , and triazole derivatives , , , , and showed the highest antitrypanosomal activity with IC values of 17.89, 1.82, 10.38, 10.26, 11.77, 9.29, 3.93, 2.11, and 0.93 μM, respectively. Compounds and showed the most potent activity against amastigotes with IC values of 18.28 and 10.54 μM, respectively. Compound showed the most potent activity against macrophage internalized amastigotes with an IC value of 8.32 μM. Conjugate triazoles displayed potential antimalarial activity against chloroquine-resistant W2 and chloroquine sensitive D6 strains (IC value range from 0.58 to 8.36 μM). Compound showed antibacterial activity against , MRSA and with IC values of 15.53, 14.22 and 47.45 μM, respectively. None of the compounds exhibited antifungal activity.
研究了一系列具有有趣生物活性骨架的异恶唑和三唑衍生物的抗菌、抗真菌和抗原虫活性。这些化合物表现出的抗锥虫活性与用于治疗人类非洲锥虫病的药物二氟甲基鸟氨酸(DMFO)相当。异恶唑类似物 、 以及三唑衍生物 、 、 、 、 和 表现出最高的抗锥虫活性,IC值分别为17.89、1.82、10.38、10.26、11.77、9.29、3.93、2.11和0.93μM。化合物 和 对无鞭毛体表现出最强的活性,IC值分别为18.28和10.54μM。化合物 对巨噬细胞内化的无鞭毛体表现出最强的活性,IC值为8.32μM。共轭三唑 对氯喹耐药的W2和氯喹敏感的D6菌株显示出潜在的抗疟活性(IC值范围为0.58至8.36μM)。化合物 对 、耐甲氧西林金黄色葡萄球菌(MRSA)和 表现出抗菌活性,IC值分别为15.53、14.22和47.45μM。这些化合物均未表现出抗真菌活性。